154106-92-0
| 中文名称 | 154106-92-0 |
|---|---|
| 中文同义词 | 化合物 T16797;化合物 RPR104632 |
| 英文名称 | RPR 104632 |
| 英文同义词 | RPR 104632;2H-1,2,4-Benzothiadiazine-3-carboxylic acid, 2-[(3-bromophenyl)methyl]-6,8-dichloro-3,4-dihydro-, 1,1-dioxide;RPR104632,RPR-104632 |
| CAS号 | 154106-92-0 |
| 分子式 | C15H11BrCl2N2O4S |
| 分子量 | 466.13 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 154106-92-0.mol |
| 结构式 | ![]() |
154106-92-0 性质
| 沸点 | 658.6±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.788±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 2.00±0.20(Predicted) |
RPR104632 antagonizes the binding of [ 3 H]5,7-dichlorokynurenic acid to the rat cerebral cortex, with a K i of 4.9 nM. RPR104632 inhibits [ 3 H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([ 3 H]TCP) binding in the presence of N-methyl-D-aspartate (NMDA) (IC 50 = 55 nM). RPR104632 inhibits the NMDA-evoked increase in guanosine 3',5'-cyclic monophosphate (cGMP) levels of neonatal rat cerebellar slices (IC 50 = 890 nM) in a non-competitive manner and markedly reduces NMDA-induced neurotoxicity in rat hippocampal slices and in cortical primary cell cultures. MK-801 (1 μM) completely protects the CA1 and CA3 pyramidal neurones against NMDA-induced toxicity, but these effects are not blocked by glycine. RPR104632 produces a significant and consistent neuroprotective effect towards all the NMDA-induced toxicity and has no effect when it is added alone at concentrations up to 10 μM. RPR104632 has neuroprotective potencies, with EC 50 of 4 μM.
